Monday, April 21, 2014

Publication utilizes PolyVivo AK09 as delivery system for photoactivated prodrug

Recent publication from University of Oklahoma utilized Polyvivo AK09 (mPEG-PLA)(www.polyscitech.com) as a delivery system for their custom synthesized prodrug Pc-(L-CA4)2 which activates upon exposure to red light.  This system successfully ablated tumors in a mouse model. Read more:  Bio, Moses, Pallavi Rajaputra, Gregory Nkepang, and Youngjae You. "A Far-Red Light Activatable, Multi-Functional Prodrug for Fluorescence Optical Imaging and Combinational Treatment." Journal of medicinal chemistry(2014).  http://pubs.acs.org/doi/abs/10.1021/jm5000722


“ABSTRACT: We recently developed “photo-unclick chemistry”, a novel chemical tool involving the cleavage of aminoacrylate by singlet oxygen, and demonstrated its application to visible light-activatable prodrugs. In this study, we prepared an advanced multifunctional prodrug, Pc-(L-CA4)2, composed of the fluorescent photosensitizer phthalocyanine (Pc), an SO-labile aminoacrylate linker (L), and a cytotoxic drug combretastatin A-4 (CA4). Pc-(L-CA4)2 had reduced dark toxicity compared with CA4. However, once illuminated, it showed improved toxicity similar to CA4 and displayed bystander effects in vitro. We monitored the time-dependent distribution of Pc-(L-CA4)2 using optical imaging with live mice. We also effectively ablated tumors by the illumination with far-red light to the mice, presumably through the combined effects of photodynamic therapy (PDT) and released chemotherapy drug, without any sign of acute systemic toxicity.”


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